Abstract
Hydroxypyridinones (HPs) are a family of N-heterocyclic metal chelators, which have been an attractive target in the development of a variety of new pharmaceutical drugs, due to their high metal chelating efficacy/specificity and easy derivatization to tune the desired biological properties. In fact, along the last decades, hydroxypyridinone derivatives, but mostly 3-hydroxy-4-pyridinone (3,4-HP), have been intensively used in drug design, following either a multitarget approach, in which one chelating unity is extrafunctionalized (hybridized) to enable the interaction with other important specific biological sites, or a polydenticity approach, in which more than one chelating moiety is conveniently attached to one scaffold, to increase the metal chelating efficacy. This review represents an update of the most recent publications (2014-2016) in mono-HP hybrids, namely as potential anti-Alzheimer's drugs, inhibitors of metalloenzymes and anti-microbials, and also polychelating compounds (poly- HP), in view of potential application, such as anti-microbial/biostatic agents, luminescent biosensors or diagnostic agents.
Keywords: Hydroxypyridinones, 3-hydroxy-4-pyridinones, iron chelators, anti-neurodegeneratives, bioinorganic medicinal chemistry.
Current Medicinal Chemistry
Title:Hydroxypyridinone Derivatives: A Fascinating Class of Chelators with Therapeutic Applications - An Update
Volume: 25 Issue: 1
Author(s): Sílvia Chaves, Luca Piemontese, Asha Hiremathad and M. Amélia Santos*
Affiliation:
- Centro de Quimica Estrutural, Instituto Superior Tecnico, Universidade de Lisboa, Av. Rovisco Pais 1, 1049-001 Lisboa,Portugal
Keywords: Hydroxypyridinones, 3-hydroxy-4-pyridinones, iron chelators, anti-neurodegeneratives, bioinorganic medicinal chemistry.
Abstract: Hydroxypyridinones (HPs) are a family of N-heterocyclic metal chelators, which have been an attractive target in the development of a variety of new pharmaceutical drugs, due to their high metal chelating efficacy/specificity and easy derivatization to tune the desired biological properties. In fact, along the last decades, hydroxypyridinone derivatives, but mostly 3-hydroxy-4-pyridinone (3,4-HP), have been intensively used in drug design, following either a multitarget approach, in which one chelating unity is extrafunctionalized (hybridized) to enable the interaction with other important specific biological sites, or a polydenticity approach, in which more than one chelating moiety is conveniently attached to one scaffold, to increase the metal chelating efficacy. This review represents an update of the most recent publications (2014-2016) in mono-HP hybrids, namely as potential anti-Alzheimer's drugs, inhibitors of metalloenzymes and anti-microbials, and also polychelating compounds (poly- HP), in view of potential application, such as anti-microbial/biostatic agents, luminescent biosensors or diagnostic agents.
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Chaves Sílvia , Piemontese Luca , Hiremathad Asha and Santos Amélia M. *, Hydroxypyridinone Derivatives: A Fascinating Class of Chelators with Therapeutic Applications - An Update, Current Medicinal Chemistry 2018; 25 (1) . https://dx.doi.org/10.2174/0929867324666170330092304
DOI https://dx.doi.org/10.2174/0929867324666170330092304 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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